Tìm theo
Etanercept
Các tên gọi khác (7 ) :
  • CD120b
  • p75
  • p80 TNF-alpha receptor
  • TNF-R2
  • Tumor necrosis factor receptor 2
  • Tumor necrosis factor receptor superfamily member 1B precursor
  • Tumor necrosis factor receptor type II
Thuốc giảm miễn dịch
Thuốc Gốc
Biotech
CAS: 185243-69-0
ATC: L04AB01
ĐG : Amgen Inc. , http://www.amgen.com
CTHH: C2224H3475N621O698S36
PTK: 51234.9000
Dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. Etanercept is produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system. It consists of 934 amino acids
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C2224H3475N621O698S36
Phân tử khối
51234.9000
Độ tan chảy
71 °C (whole mAb)
Độ kỵ nước
-0.529
Điểm đẳng điện tích
7.89
Dược Lực Học : Tumor necrosis factor TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. Elevated levels of TNF are found in tissues and fluids of patients with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis (AS), and plaque psoriasis. Etanercept binds specifically to tumor necrosis factor (TNF) and blocks its interaction with cell surface TNF receptors.
Cơ Chế Tác Dụng : Dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. Etanercept is produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system. It consists of 934 amino acids There are two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75). The biological activity of TNF is dependent upon binding to either cell surface receptor (p75 or p55). Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecules, thereby effectively removing them from circulation.
Dược Động Học :
▧ Absorption :
Bioavailability following sub-Q administration is approximately 60%. Peak plasma concentrations achieved within 69 hours.
▧ Half Life :
102 +/- 30 hrs in individuals with rheumatoid arthritis and 68 hours in healthy adults
▧ Clearance :
* 160 +/- 80 mL/hr [RA patients]
Chỉ Định : For treatment of severe active rheumatoid arthritis in adults, severe juvenile idiopathic arthritis, ankylosing spondylitis, and severe plaque psoriasis.
Tương Tác Thuốc :
  • Abatacept Avoid combination because of increased adverse effects of Abatacept.
  • Anakinra Avoid combination due to increased adverse effects of anakinra and increased risk of infections.
  • Belimumab Avoid combination because of enhanced adverse effects of belimumab.
  • Belimumab Avoid combination due to enhanced toxic effects of belimumab.
  • Canakinumab Combination should be avoided because Etanercept increase the toxic effects of canakinumab including neutropenia.
  • Certolizumab pegol Avoid combination as certolizumab pegol toxic effects would be enhanced.
  • Cyclophosphamide Avoid combination due to enhanced adverse effects of cyclophosphasmide and increased risk of solid cancer development.
  • Denosumab Monitor therapy as there may be an enhanced immunosuppressive effect.
  • Infliximab Avoid combination because etanercept may increase immunosuppressive effects of infliximab.
  • Leflunomide Consider modifying therapy due to enhanced adverse effects of leflunomide including hematologic toxicity.
  • Natalizumab Avoid combination due to enhanced adverse effects of natalizumab and increased risk of infections.
  • Pimecrolimus Avoid combination due to enhanced immunosuppressive effects.
  • Rilonacept results in increased immunosuppressive effects; increases the risk of infection.
  • Roflumilast Due to enhanced immunosuppressive effects, therapy modification should be considered.
  • Sipuleucel-T Monitor therapy because of reduced therapeutic effect of sipuleucel-T.
  • Tacrolimus Avoid combination due to enhanced immunosuppressive effects
  • Tocilizumab Avoid combination due to enhanced immunosuppressive effects.
  • Tofacitinib Etanercept increases the risk of added immunosuppression. It is recommended to avoid concurrent therapy.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Solution - Subcutaneous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Immunex Corp
    Sản phẩm biệt dược : Enbrel
  • Công ty :
    Sản phẩm biệt dược : Enbrel Sureclick
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00005
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07897
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00742
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/58406-455-04
GenBank
http://www.ncbi.nlm.nih.gov/nuccore/M32315
PharmGKB
http://www.pharmgkb.org/drug/PA449515
Wikipedia
http://en.wikipedia.org/wiki/Etanercept
RxList
http://www.rxlist.com/cgi/generic/etanercept.htm
Drugs.com
http://www.drugs.com/cdi/etanercept.html
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